Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Treating obesity with muscarinic receptor M1 antagonists

a technology of muscarinic receptor and m1 antagonist, which is applied in the field of obesity treatment, can solve the problems of not being able to disclose or suggest the ability of pirenzepine to interfere with lipogenic sensitivity or facilitate weight loss, and not being able to have psychotropic effects. psychotropic effect or other problems

Inactive Publication Date: 2014-06-10
THERAKOS INC
View PDF30 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes methods for treating obesity, suppressing appetite, promoting weight loss, and preventing weight gain by using a medication that blocks a specific receptor in the body called M1R. The medication can be used alone or in combination with other drugs such as antidepressants or anti-obesity agents. The technical effects of this invention include promoting weight loss and maintaining a stable weight, as well as preventing or reducing unwanted weight gain.

Problems solved by technology

While pirenzepine and telenzepine are structurally similar to tricyclic antidepressants such as imipramine, they are not known to have psychotropic effects when taken orally for the treatment of peptic ulcer disease.
In addition, in earlier studies of mice and rats, pirenzepine administered systemically failed to elicit any behavioral effects (see, Rogoz, Z., Skuza, G., Sowinska, H., Pol. J. Pharmacol. Pharm., 1981, vol.
Bevan related the timing of administration of pirenzepine with the timing of a meal, but does not disclose or suggest the ability of pirenzepine to interfere with lipogenic sensitivity or its use in facilitating weight loss.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Treating obesity with muscarinic receptor M<sub>1 </sub>antagonists
  • Treating obesity with muscarinic receptor M<sub>1 </sub>antagonists
  • Treating obesity with muscarinic receptor M<sub>1 </sub>antagonists

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0169]Appetite Suppression: Three-month-old (300-350 grams) male, Sprague-Dawley rats (individually housed) were used to assess compounds for their appetite suppressant effects. Rats were acclimatized to a “high fat” food diet (BioServ Diet #F3282 or Research Diets #12451) for two weeks prior to testing (access to food and water ad libitum). One day prior to the experiment (at 5:00 PM), food was removed from the cages in order to motivate feeding when the food was returned the following morning (water remained available throughout the experiment). Prior to presentation of the food, rats (n=8-10 / dose group) were dosed intraperitoneally (ip) or orally (po) with the compound under investigation, returned to their home cage and immediately given a pre-weighed amount of food. Four hours after administration, the food was removed from the cage, weighed, recorded (4-Hour Consumption) and returned to the rat until the following morning. Twenty-four hours after administration, the remaining ...

example 2

[0178]Reduction in Weight Gain: Three- to four-month-old (475-550 grams) male, Sprague-Dawley rats (individually housed) were used to assess compounds for their ability to prevent weight gain. At the onset of chronic experiments, rats had been maintained (ad libitum access) on a “high fat” diet (BioServ Diet #F3282 or Research Diets #12451) for approximately one month. Individual body weights and water consumptions were recorded three times per week throughout the duration of the experiment. After approximately two weeks of data collection, rats were counter-balanced to produce treatment groups with equivalent mean body weights. Under isofluorane-induced anesthesia, rats were surgically implanted (subscapular, subcutaneous [sc] placement) with osmotic mini-pumps (Alzet 2mL2) containing the appropriate drug concentration (based on mean body weights and calculated durations of delivery). Alternatively, for studies using the oral route of administration, rats were dosed by gavage daily...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
timeaaaaaaaaaa
half timeaaaaaaaaaa
weightaaaaaaaaaa
Login to View More

Abstract

Provided are methods of treating obesity and effecting desired weight loss or preventing undesired weight gain by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The preferential muscarinic acetylcholine receptor M1 antagonist, optionally can be administered with an anti-obesity agent, for example, an anorexiant. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application No. 60 / 805,066, filed Jun. 16, 2006 and U.S. Provisional Application No. 60 / 829,225, filed Oct. 12, 2006, the entire disclosures of both of which are hereby incorporated herein by reference.STATEMENT AS TO RIGHTS TO INVENTIONS MADE UNDER FEDERALLY SPONSORED RESEARCH AND DEVELOPMENT[0002]Not ApplicableFIELD OF THE INVENTION[0003]The present invention relates to the treatment of obesity and the facilitation of weight loss by administration of a selective M1 muscarinic receptor (M1R) antagonist, alone or in combination with an antidepressant.BACKGROUND OF THE INVENTION[0004]The neurotransmitter acetylcholine (ACh) interacts with two types of receptors in effector cell membranes: nicotinic receptors (nAChR), which are ligand-gated ion channels, and muscarinic receptors (mAChR), which are G protein-coupled receptors. In mammals five subtypes of mAChR, designated M1 to M5, have...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(United States)
IPC IPC(8): C07D487/04A61K31/135C07D307/80A61K31/55C07D333/20
CPCA61K31/381A61K31/137A61K45/06A61K31/551A61K31/55A61K31/343A61K31/5513A61K31/135A61P25/24A61P3/04A61P3/06A61P43/00A61K2300/00
Inventor SEED, BRIANMECHANIC, JORDAN
Owner THERAKOS INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com